GABAA receptor subtype selectivity underlying selective anxiolytic effect of baicalin

  title={GABAA receptor subtype selectivity underlying selective anxiolytic effect of baicalin},
  author={Feng Wang and Zhiwen Xu and Lihuan Ren and Shui Ying Tsang and Hong Xue},
Flavonoids as GABAA receptor ligands: the whole story?
Flavonoids are prominent drugs in the treatment of mental disorders, and can also be used as tools to study modulatory sites at GABA type A receptors and to develop GABAtype A selective agents further.
Recent developments in potential anxiolytic agents targeting GABAA/BzR complex or the translocator protein (18kDa) (TSPO).
Putative compounds affecting the GABAergic system which may provide the basis for fast acting anxiolytics with a favorable side effect profile are discussed.
Effects of flavone 6-substitutions on GABAA receptors efficacy.
The Anticonvulsant and Neuroprotective Effects of Baicalin on Pilocarpine-Induced Epileptic Model in Rats
Pretreatment with baicalin significantly delayed the onset of the first limbic seizures and SE, reduced the mortality rate, and attenuated the changes in the levels of lipid peroxidation, nitrite content and reduced glutathione in the hippocampus of pilocarpine-treated rats, indicating remarkable anticonvulsant and neuroprotective effects of baicalsin.
Effects of a Flavonoid-Rich Fraction on the Acquisition and Extinction of Fear Memory: Pharmacological and Molecular Approaches
It is shown for the first time that the serotoninergic and glutamatergic receptors are important targets for the effect of FfB on the conditioned fear and spontaneous recovery, in which the ERK signaling pathway appears to be modulated.
(+)‐Dehydrofukinone modulates membrane potential and delays seizure onset by GABAa receptor‐mediated mechanism in mice


GABA-A receptors: a viable target for novel anxiolytics?
  • P. Whiting
  • Biology, Psychology
    Current opinion in pharmacology
  • 2006
Evidence for a Significant Role of α3-Containing GABAA Receptors in Mediating the Anxiolytic Effects of Benzodiazepines
Data show that potentiation of α3-containing GABAA receptors is sufficient to produce the anxiolytic effects of BZs and that α2 potentiation may not be necessary.
Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype
This work created genetically modified mice with a diazepam-insensitive α1 subtype and a selective BZ site ligand to explore GABAA receptor subtypes mediating specific physiological effects and revealed that the α1Subtype mediated the sedative, but not the anxiolytic effects of benzodiazepines.
Anxiolytic-Like Effect of baicalin and its additivity with other anxiolytics.
The potential of baicalin as a candidate anxiolytic and its possible application in multidrug therapy is demonstrated and motor-depressive and myorelaxant side effects commonly associated with anxIOlytics were not observed with baical in at effective anxiolyntic doses.
Neuroactive flavonoids interacting with GABAA receptor complex.
Findings from structure-activity relationship (SAR) studies guided the identification of several synthetic flavonoids with high BZ-site binding affinity and in vivo activity, and further quantitative SAR studies resulted in the development of several pharmacophore models.
Benzodiazepine actions mediated by specific γ-aminobutyric acidA receptor subtypes
GABAA (γ-aminobutyric acidA) receptors are molecular substrates for the regulation of vigilance, anxiety, muscle tension, epileptogenic activity and memory functions, which is evident from the
A new benzodiazepine pharmacology.
Rational drug targeting to specific receptor subtypes has now become possible, and only restricted neuronal networks will be modulated by the new subtype-selective drugs.
GABA(A)-receptor subtypes: clinical efficacy and selectivity of benzodiazepine site ligands.
Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are seen in the clinical use of benzodiazepines.